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Identification
NameFluvastatin
Accession NumberDB01095  (APRD00346)
TypeSmall Molecule
GroupsApproved
DescriptionFluvastatin is an antilipemic agent that competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Fluvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease. It is also the first entirely synthetic HMG-CoA reductase inhibitor and is structurally distinct from the fungal derivatives of this therapeutic class.
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Fluvastatin Sodium ERtablet, extended release80 mg/1oralSandoz Inc2015-10-16Not applicableUs
Lescolcapsule20 mg/1oralNovartis Pharmaceuticals Corporation1993-12-30Not applicableUs
Lescolcapsule20 mg/1oralPhysicians Total Care, Inc.1994-06-10Not applicableUs
Lescolcapsule40 mg/1oralNovartis Pharmaceuticals Corporation1993-12-30Not applicableUs
Lescolcapsule40 mg/1oralPhysicians Total Care, Inc.2002-03-08Not applicableUs
Lescol 20mgcapsule20 mgoralNovartis Pharmaceuticals Canada Inc1994-12-31Not applicableCanada
Lescol 40mgcapsule40 mgoralNovartis Pharmaceuticals Canada Inc1994-12-31Not applicableCanada
Lescol XLtablet, extended release80 mg/1oralCarilion Materials Management2000-10-06Not applicableUs
Lescol XLtablet, extended release80 mg/1oralNovartis Pharmaceuticals Corporation2000-10-06Not applicableUs
Lescol XLtablet, extended release80 mg/1oralPhysicians Total Care, Inc.2002-03-12Not applicableUs
Lescol XLtablet (extended-release)80 mgoralNovartis Pharmaceuticals Canada Inc2004-04-05Not applicableCanada
Sandoz Fluvastatincapsule20 mgoralSandoz Canada Incorporated2013-02-15Not applicableCanada
Sandoz Fluvastatincapsule40 mgoralSandoz Canada Incorporated2013-02-15Not applicableCanada
Teva-fluvastatincapsule20 mgoralTeva Canada Limited2012-12-11Not applicableCanada
Teva-fluvastatincapsule40 mgoralTeva Canada Limited2012-12-11Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Fluvastatincapsule20 mg/1oralTeva Pharmaceuticals USA Inc2012-07-05Not applicableUs
Fluvastatincapsule40 mg/1oralTeva Pharmaceuticals USA Inc2012-07-05Not applicableUs
Fluvastatin Sodiumcapsule40 mg/1oralMylan Pharmaceuticals Inc.2013-03-19Not applicableUs
Fluvastatin Sodiumcapsule20 mg/1oralCarilion Materials Management2013-03-19Not applicableUs
Fluvastatin Sodiumtablet, film coated, extended release80 mg/1oralMylan Pharmaceuticals Inc.2015-09-11Not applicableUs
Fluvastatin Sodiumcapsule40 mg/1oralCarilion Materials Management2013-03-19Not applicableUs
Fluvastatin Sodiumcapsule20 mg/1oralMylan Pharmaceuticals Inc.2013-03-19Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CanefAstraZeneca
CranocAstellas
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Fluvastatin Sodium
Thumb
  • InChI Key: ZGGHKIMDNBDHJB-UHFFFAOYNA-M
  • Monoisotopic Mass: 433.166531173
  • Average Mass: 433.4478
DBSALT000088
Categories
UNII4L066368AS
CAS number93957-54-1
WeightAverage: 411.4659
Monoisotopic: 411.18458653
Chemical FormulaC24H26FNO4
InChI KeyInChIKey=FJLGEFLZQAZZCD-NDDZYTDBNA-N
InChI
InChI=1/C24H26FNO4/c1-15(2)26-21-6-4-3-5-20(21)24(16-7-9-17(25)10-8-16)22(26)12-11-18(27)13-19(28)14-23(29)30/h3-12,15,18-19,27-28H,13-14H2,1-2H3,(H,29,30)/b12-11+/t18-,19-/s2
IUPAC Name
(3R,5S,6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
SMILES
CC(C)N1C(\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)=C(C2=CC=CC=C12)C1=CC=C(F)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpyrroles. These are polycyclic aromatic compounds containing a benzene ring linked to a pyrrole ring through a CC or CN bond.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyrroles
Sub ClassSubstituted pyrroles
Direct ParentPhenylpyrroles
Alternative Parents
Substituents
  • 3-phenylpyrrole
  • Medium-chain hydroxy acid
  • Indole or derivatives
  • Indole
  • Medium-chain fatty acid
  • Heterocyclic fatty acid
  • Halogenated fatty acid
  • Halobenzene
  • Fluorobenzene
  • Beta-hydroxy acid
  • Fatty acyl
  • Fatty acid
  • Benzenoid
  • Unsaturated fatty acid
  • Hydroxy acid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Secondary alcohol
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
  • (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (CHEBI:38565 )
Pharmacology
IndicationTo be used as an adjunct to dietary therapy to prevent cardiovascular events. May be used as secondary prevention in patients with coronary heart disease (CHD) to reduce the risk of requiring coronary revascularization procedures, for reducing progression of coronary atherosclerosis in hypercholesterolemic patients with CHD, and for the treatment of primary hypercholesterolemia and mixed dyslidipidemia.
PharmacodynamicsFluvastatin, the first synthetically-derived HMG-CoA reductase inhibitor, is a hydrophilic, acidic, antilipemic agent used to lower cholesterol and triglyceride levels associated with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson types IIa and IIb), to slow the progression of coronary atherosclerosis in patients with CHD and as secondary prevention therapy in patients with CHD to reduce the risk of requiring coronary revascularization procedures. Although similar to lovastatin, simvastatin, and pravastatin, fluvastatin has a shorter half-life, no active metabolites, extensive protein binding, and minimal CSF penetration. Fluvastatin acts primarily in the liver. It is prepared as a racemate of two erythro enantiomers of which the 3R,5S enantiomer exerts the pharmacologic effect.
Mechanism of actionFluvastatin selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, the rate-limiting step in cholesterol biosynthesis. Inhibition results in a decrease in hepatic cholesterol levels which stimulates the synthesis of LDL receptors and increases hepatic uptake of LDL cholesterol. The end result is decreased levels of plasma total and LDL cholesterol.
Related Articles
AbsorptionRapidly and almost completely absorbed (> 90%), but undergoes extensive first pass metabolism. Bioavailability is 24% (range 9-50%) when a 10 mg dose is given. The mean relative bioavailability of the extended-release tablet is 29% (range: 9% to 66%) compared to an immediate-release capsule administered under fasting conditions. When given orally, fluvastatin reaches peak concentrations (Tmax) in less than one hour. Taking the extended release tablet with a high-fat meal will delay absorption (Tmax = 6 hours) and increase bioavailability by approximately 50%. However, the maximum concentration of fluvastatin sodium extended-release tablets seen after a high fat meal is less than the peak concentration following a single dose or twice daily dose of the 40 mg fluvastatin capsule.
Volume of distribution
  • 0.35 L/kg
Protein binding98% bound to plasma proteins. At therapeutic concentrations, the protein binding of fluvastatin is not affected by warfarin, salicylic acid and glyburide.
Metabolism

Undergoes hepatic metabolism primarily via hydroxylation of the indole ring at the 5- and 6-positions to 5-hydroxy fluvastatin and 6-hydroxy fluvastatin, respectively. N-dealkylation to N-desisopropyl fluvastatin and beta-oxidation of the side chain also occurs. Metabolized primarily by the CYP2C9 isozyme system (75%), and to a lesser extent by CYP3A4 (~20%) and CYP2C8 (~5%). Hydroxylated metabolites retain some pharmcological activity, but are present as conjugates (glucuronides and sulfates) in the blood and are rapidly eliminated via bile into feces. Both enantiomers of fluvastatin are metabolized in a similar manner. Fluvastatin also undergoes glucuronidation via UGT enzymes.

SubstrateEnzymesProduct
Fluvastatin
6-HydroxyfluvastatinDetails
Fluvastatin
N-Deisopropyl-fluvastatinDetails
Fluvastatin
5-HydroxyfluvastatinDetails
Route of eliminationWhen orally administered, fluvastatin is primarily excreted in the faces ( ~90%) as metabolites, with less than 2% present as unchanged drug. Approximately 5% was recovered in the urine.
Half life3 hours
Clearance
  • 0.8 L/h/kg
  • 107 ± 38.1 L/h [Hypercholesterolemia patients receiving a single dose of 20 mg]
  • 87.8 ± 45 L/h [Hypercholesterolemia patients receiving 20 mg twice daily]
  • 108 ± 44.7 L/h [Hypercholesterolemia patients receiving 40 mg single]
  • 64.2 ± 21.1 L/h [Hypercholesterolemia patients receiving 40 mg twice daily]
ToxicityGenerally well-tolerated. May cause gastrointestinal upset (diarrhea, nausea, constipation, gas, abdominal pain), myotoxicity (mypothy, myositis, rhabdomyolysis), and hepatotoxicity.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Fluvastatin Action PathwayDrug actionSMP00119
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9943
Blood Brain Barrier+0.9382
Caco-2 permeable-0.5053
P-glycoprotein substrateNon-substrate0.5176
P-glycoprotein inhibitor INon-inhibitor0.7395
P-glycoprotein inhibitor IINon-inhibitor0.8381
Renal organic cation transporterNon-inhibitor0.8823
CYP450 2C9 substrateNon-substrate0.7305
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.6111
CYP450 1A2 substrateNon-inhibitor0.6003
CYP450 2C9 inhibitorNon-inhibitor0.675
CYP450 2D6 inhibitorNon-inhibitor0.8983
CYP450 2C19 inhibitorNon-inhibitor0.6314
CYP450 3A4 inhibitorNon-inhibitor0.8811
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.809
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7909
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.9472 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9899
hERG inhibition (predictor II)Non-inhibitor0.848
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseoral80 mg/1
Capsuleoral20 mg/1
Capsuleoral40 mg/1
Capsuleoral20 mg
Capsuleoral40 mg
Tablet (extended-release)oral80 mg
Tablet, extended releaseoral80 mg/1
Prices
Unit descriptionCostUnit
Lescol XL 80 mg 24 Hour tablet4.25USD tablet
Lescol xl 80 mg tablet4.24USD tablet
Lescol xl 80 mg tablet sa3.66USD tablet
Lescol 20 mg capsule3.38USD capsule
Lescol 40 mg capsule3.37USD capsule
Lescol Xl 80 mg Extended-Release Tablet1.62USD tablet
Lescol 40 mg Capsule1.35USD capsule
Lescol 20 mg Capsule0.96USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2085037 No2000-11-282012-12-10Canada
CA2346868 No2008-09-092019-10-12Canada
US5354772 No1994-10-112011-10-11Us
US6242003 Yes2000-10-132020-10-13Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point194-197 °CNot Available
water solubility0.46 mg/LNot Available
logP4.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00441 mg/mLALOGPS
logP3.69ALOGPS
logP3.83ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)4.56ChemAxon
pKa (Strongest Basic)-2.8ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area82.69 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity114.86 m3·mol-1ChemAxon
Polarizability43.9 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Gustavo Frenkel, Eyal Gilboa, “Process for the preparation of fluvastatin sodium crystal form XIV.” U.S. Patent US20050119342, issued June 02, 2005.

US20050119342
General References
  1. Toda T, Eliasson E, Ask B, Inotsume N, Rane A: Roles of different CYP enzymes in the formation of specific fluvastatin metabolites by human liver microsomes. Basic Clin Pharmacol Toxicol. 2009 Nov;105(5):327-32. doi: 10.1111/j.1742-7843.2009.00453.x. Epub 2009 Aug 6. [PubMed:19663817 ]
External Links
ATC CodesC10AA04
AHFS Codes
  • 24:06.08
PDB EntriesNot Available
FDA labelDownload (84.5 KB)
MSDSDownload (101 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Fluvastatin can be increased when it is combined with Abiraterone.
AceclofenacThe metabolism of Aceclofenac can be decreased when combined with Fluvastatin.
AcenocoumarolFluvastatin may increase the anticoagulant activities of Acenocoumarol.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Fluvastatin.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be decreased when combined with Fluvastatin.
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Fluvastatin.
AlosetronThe metabolism of Alosetron can be decreased when combined with Fluvastatin.
AlprazolamThe metabolism of Alprazolam can be decreased when combined with Fluvastatin.
Aluminum hydroxideThe serum concentration of Fluvastatin can be decreased when it is combined with Aluminum hydroxide.
Aluminum phosphateThe serum concentration of Fluvastatin can be decreased when it is combined with Aluminum phosphate.
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Fluvastatin.
AmiodaroneThe metabolism of Fluvastatin can be decreased when combined with Amiodarone.
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Fluvastatin.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Fluvastatin.
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Fluvastatin.
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Fluvastatin.
ApixabanThe metabolism of Apixaban can be decreased when combined with Fluvastatin.
AprepitantThe serum concentration of Fluvastatin can be increased when it is combined with Aprepitant.
Arachidonic AcidThe metabolism of Arachidonic Acid can be decreased when combined with Fluvastatin.
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Fluvastatin.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Fluvastatin.
ArtemetherThe metabolism of Fluvastatin can be decreased when combined with Artemether.
AtazanavirThe serum concentration of Fluvastatin can be increased when it is combined with Atazanavir.
AtazanavirThe metabolism of Atazanavir can be decreased when combined with Fluvastatin.
AtomoxetineThe metabolism of Fluvastatin can be decreased when combined with Atomoxetine.
AzelastineThe metabolism of Azelastine can be decreased when combined with Fluvastatin.
BetaxololThe metabolism of Fluvastatin can be decreased when combined with Betaxolol.
BexaroteneThe serum concentration of Fluvastatin can be decreased when it is combined with Bexarotene.
BexaroteneThe metabolism of Bexarotene can be decreased when combined with Fluvastatin.
BezafibrateBezafibrate may increase the myopathic rhabdomyolysis activities of Fluvastatin.
Bismuth SubcitrateThe serum concentration of Fluvastatin can be decreased when it is combined with Bismuth Subcitrate.
BoceprevirThe serum concentration of Fluvastatin can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Fluvastatin can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Fluvastatin can be decreased when it is combined with Bosentan.
BosentanThe serum concentration of Bosentan can be increased when it is combined with Fluvastatin.
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Fluvastatin.
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Fluvastatin.
BupropionThe metabolism of Fluvastatin can be decreased when combined with Bupropion.
CabozantinibThe metabolism of Cabozantinib can be decreased when combined with Fluvastatin.
CaffeineThe metabolism of Caffeine can be decreased when combined with Fluvastatin.
Calcium carbonateThe serum concentration of Fluvastatin can be decreased when it is combined with Calcium carbonate.
CandesartanThe metabolism of Candesartan can be decreased when combined with Fluvastatin.
CapecitabineThe metabolism of Fluvastatin can be decreased when combined with Capecitabine.
CarbamazepineThe metabolism of Fluvastatin can be increased when combined with Carbamazepine.
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Fluvastatin.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Fluvastatin.
CelecoxibThe metabolism of Fluvastatin can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Fluvastatin can be increased when it is combined with Ceritinib.
ChloroquineThe metabolism of Fluvastatin can be decreased when combined with Chloroquine.
ChlorpromazineThe metabolism of Fluvastatin can be decreased when combined with Chlorpromazine.
ChlorpropamideThe metabolism of Chlorpropamide can be decreased when combined with Fluvastatin.
CholecalciferolThe metabolism of Fluvastatin can be decreased when combined with Cholecalciferol.
CholestyramineThe serum concentration of Fluvastatin can be decreased when it is combined with Cholestyramine.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Fluvastatin.
CimetidineThe metabolism of Fluvastatin can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Fluvastatin can be decreased when combined with Cinacalcet.
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Fluvastatin.
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Fluvastatin.
CisaprideThe metabolism of Cisapride can be decreased when combined with Fluvastatin.
CitalopramThe metabolism of Fluvastatin can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Fluvastatin can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Fluvastatin can be decreased when combined with Clemastine.
ClobazamThe metabolism of Fluvastatin can be decreased when combined with Clobazam.
ClomipramineThe metabolism of Fluvastatin can be decreased when combined with Clomipramine.
ClopidogrelThe metabolism of Clopidogrel can be decreased when combined with Fluvastatin.
ClotrimazoleThe metabolism of Fluvastatin can be decreased when combined with Clotrimazole.
ClozapineThe metabolism of Fluvastatin can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Fluvastatin can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Fluvastatin can be decreased when combined with Cocaine.
ColchicineColchicine may increase the myopathic rhabdomyolysis activities of Fluvastatin.
ConivaptanThe serum concentration of Fluvastatin can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Fluvastatin can be decreased when combined with Crizotinib.
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Fluvastatin.
CyclosporineThe metabolism of Fluvastatin can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Fluvastatin can be increased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Fluvastatin can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Fluvastatin can be increased when it is combined with Daclatasvir.
DanazolThe serum concentration of Fluvastatin can be increased when it is combined with Danazol.
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Fluvastatin.
DapsoneThe metabolism of Dapsone can be decreased when combined with Fluvastatin.
DaptomycinThe risk or severity of adverse effects can be increased when Fluvastatin is combined with Daptomycin.
DarifenacinThe metabolism of Fluvastatin can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Fluvastatin can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Fluvastatin can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Fluvastatin can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Fluvastatin can be decreased when combined with Delavirdine.
DesipramineThe metabolism of Fluvastatin can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Fluvastatin can be decreased when it is combined with Dexamethasone.
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Fluvastatin.
DiazepamThe metabolism of Diazepam can be decreased when combined with Fluvastatin.
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Fluvastatin.
DicoumarolFluvastatin may increase the anticoagulant activities of Dicoumarol.
DihydroergotamineThe metabolism of Fluvastatin can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Fluvastatin can be decreased when combined with Diltiazem.
DiphenhydramineThe metabolism of Fluvastatin can be decreased when combined with Diphenhydramine.
DolasetronThe metabolism of Dolasetron can be decreased when combined with Fluvastatin.
DonepezilThe metabolism of Donepezil can be decreased when combined with Fluvastatin.
DopamineThe metabolism of Dopamine can be decreased when combined with Fluvastatin.
DorzolamideThe metabolism of Dorzolamide can be decreased when combined with Fluvastatin.
DoxepinThe metabolism of Doxepin can be decreased when combined with Fluvastatin.
DoxycyclineThe metabolism of Fluvastatin can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Fluvastatin.
DronedaroneThe metabolism of Fluvastatin can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Fluvastatin can be decreased when combined with Duloxetine.
EfavirenzThe serum concentration of Fluvastatin can be decreased when it is combined with Efavirenz.
EletriptanThe metabolism of Eletriptan can be decreased when combined with Fluvastatin.
EliglustatThe metabolism of Fluvastatin can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Fluvastatin can be decreased when it is combined with Enzalutamide.
EpoprostenolThe metabolism of Epoprostenol can be decreased when combined with Fluvastatin.
ErythromycinThe metabolism of Fluvastatin can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Fluvastatin can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe metabolism of Estradiol can be decreased when combined with Fluvastatin.
EstroneThe metabolism of Estrone can be decreased when combined with Fluvastatin.
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Fluvastatin.
Ethyl biscoumacetateFluvastatin may increase the anticoagulant activities of Ethyl biscoumacetate.
EtodolacThe metabolism of Etodolac can be decreased when combined with Fluvastatin.
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Fluvastatin.
EtravirineThe serum concentration of Fluvastatin can be decreased when it is combined with Etravirine.
EtravirineThe metabolism of Etravirine can be decreased when combined with Fluvastatin.
FelodipineThe metabolism of Fluvastatin can be decreased when combined with Felodipine.
FenofibrateThe risk or severity of adverse effects can be increased when Fenofibrate is combined with Fluvastatin.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Fluvastatin.
FloxuridineThe metabolism of Fluvastatin can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Fluvastatin can be decreased when combined with Fluconazole.
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Fluvastatin.
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Fluvastatin.
FluorouracilThe metabolism of Fluvastatin can be decreased when combined with Fluorouracil.
FluoxetineThe metabolism of Fluvastatin can be decreased when combined with Fluoxetine.
FlurbiprofenThe metabolism of Flurbiprofen can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Fluvastatin can be decreased when combined with Fluvoxamine.
FormoterolThe metabolism of Formoterol can be decreased when combined with Fluvastatin.
FosamprenavirThe metabolism of Fluvastatin can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Fluvastatin can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Fluvastatin can be decreased when it is combined with Fosphenytoin.
FosphenytoinThe metabolism of Fosphenytoin can be decreased when combined with Fluvastatin.
Fusidic AcidThe serum concentration of Fluvastatin can be increased when it is combined with Fusidic Acid.
GavestinelThe metabolism of Gavestinel can be decreased when combined with Fluvastatin.
GemfibrozilGemfibrozil may increase the myopathic rhabdomyolysis activities of Fluvastatin.
GliclazideThe metabolism of Gliclazide can be decreased when combined with Fluvastatin.
GlimepirideThe metabolism of Glimepiride can be decreased when combined with Fluvastatin.
GlipizideThe metabolism of Glipizide can be decreased when combined with Fluvastatin.
GlyburideThe metabolism of Glyburide can be decreased when combined with Fluvastatin.
GuanfacineThe metabolism of Guanfacine can be decreased when combined with Fluvastatin.
HaloperidolThe metabolism of Fluvastatin can be decreased when combined with Haloperidol.
HalothaneThe metabolism of Halothane can be decreased when combined with Fluvastatin.
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Fluvastatin.
Histamine PhosphateThe metabolism of Histamine Phosphate can be decreased when combined with Fluvastatin.
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Fluvastatin.
IbuprofenThe metabolism of Ibuprofen can be decreased when combined with Fluvastatin.
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Fluvastatin.
IdelalisibThe serum concentration of Fluvastatin can be increased when it is combined with Idelalisib.
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Fluvastatin.
ImatinibThe metabolism of Fluvastatin can be decreased when combined with Imatinib.
ImipramineThe metabolism of Fluvastatin can be decreased when combined with Imipramine.
IndinavirThe metabolism of Fluvastatin can be decreased when combined with Indinavir.
indisulamThe metabolism of indisulam can be decreased when combined with Fluvastatin.
IndomethacinThe metabolism of Indomethacin can be decreased when combined with Fluvastatin.
IrbesartanThe metabolism of Fluvastatin can be decreased when combined with Irbesartan.
IsavuconazoniumThe metabolism of Fluvastatin can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Fluvastatin can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Fluvastatin can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Fluvastatin can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Fluvastatin can be increased when it is combined with Ivacaftor.
IxazomibThe metabolism of Ixazomib can be decreased when combined with Fluvastatin.
KetamineThe metabolism of Ketamine can be decreased when combined with Fluvastatin.
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Fluvastatin.
KetoconazoleThe metabolism of Fluvastatin can be decreased when combined with Ketoconazole.
KetoprofenThe metabolism of Ketoprofen can be decreased when combined with Fluvastatin.
LansoprazoleThe metabolism of Lansoprazole can be decreased when combined with Fluvastatin.
Lanthanum carbonateThe serum concentration of Lanthanum carbonate can be decreased when it is combined with Fluvastatin.
LapatinibThe metabolism of Fluvastatin can be decreased when combined with Lapatinib.
LeflunomideThe metabolism of Leflunomide can be decreased when combined with Fluvastatin.
LesinuradThe metabolism of Lesinurad can be decreased when combined with Fluvastatin.
LicofeloneThe metabolism of Licofelone can be decreased when combined with Fluvastatin.
LidocaineThe metabolism of Lidocaine can be decreased when combined with Fluvastatin.
LopinavirThe metabolism of Fluvastatin can be decreased when combined with Lopinavir.
LoratadineThe metabolism of Loratadine can be decreased when combined with Fluvastatin.
LorcaserinThe metabolism of Fluvastatin can be decreased when combined with Lorcaserin.
LornoxicamThe metabolism of Lornoxicam can be decreased when combined with Fluvastatin.
LosartanThe metabolism of Fluvastatin can be decreased when combined with Losartan.
LovastatinThe metabolism of Fluvastatin can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Fluvastatin can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Fluvastatin can be decreased when it is combined with Lumacaftor.
LumefantrineThe metabolism of Fluvastatin can be decreased when combined with Lumefantrine.
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Fluvastatin.
MagaldrateThe serum concentration of Fluvastatin can be decreased when it is combined with Magaldrate.
Magnesium carbonateThe serum concentration of Fluvastatin can be decreased when it is combined with Magnesium carbonate.
Magnesium hydroxideThe serum concentration of Fluvastatin can be decreased when it is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Fluvastatin can be decreased when it is combined with Magnesium oxide.
Magnesium TrisilicateThe serum concentration of Fluvastatin can be decreased when it is combined with Magnesium Trisilicate.
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Fluvastatin.
MelatoninThe metabolism of Melatonin can be decreased when combined with Fluvastatin.
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Fluvastatin.
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Fluvastatin.
MestranolThe metabolism of Mestranol can be decreased when combined with Fluvastatin.
MethadoneThe metabolism of Fluvastatin can be decreased when combined with Methadone.
MethotrimeprazineThe metabolism of Fluvastatin can be decreased when combined with Methotrimeprazine.
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Fluvastatin.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Fluvastatin.
MetoprololThe metabolism of Fluvastatin can be decreased when combined with Metoprolol.
MetronidazoleThe metabolism of Metronidazole can be decreased when combined with Fluvastatin.
MifepristoneThe metabolism of Fluvastatin can be decreased when combined with Mifepristone.
MirabegronThe metabolism of Fluvastatin can be decreased when combined with Mirabegron.
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Fluvastatin.
MitotaneThe serum concentration of Fluvastatin can be decreased when it is combined with Mitotane.
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Fluvastatin.
ModafinilThe serum concentration of Fluvastatin can be decreased when it is combined with Modafinil.
MontelukastThe metabolism of Montelukast can be decreased when combined with Fluvastatin.
NafcillinThe serum concentration of Fluvastatin can be decreased when it is combined with Nafcillin.
NaproxenThe metabolism of Naproxen can be decreased when combined with Fluvastatin.
NateglinideThe metabolism of Nateglinide can be decreased when combined with Fluvastatin.
NefazodoneThe metabolism of Fluvastatin can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Fluvastatin can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Fluvastatin can be increased when it is combined with Netupitant.
NetupitantThe metabolism of Netupitant can be decreased when combined with Fluvastatin.
NevirapineThe metabolism of Fluvastatin can be decreased when combined with Nevirapine.
NiacinThe risk or severity of adverse effects can be increased when Niacin is combined with Fluvastatin.
NicardipineThe metabolism of Fluvastatin can be decreased when combined with Nicardipine.
NiclosamideThe metabolism of Niclosamide can be decreased when combined with Fluvastatin.
NicotinamideThe risk or severity of adverse effects can be increased when Nicotinamide is combined with Fluvastatin.
NicotineThe metabolism of Nicotine can be decreased when combined with Fluvastatin.
NilotinibThe metabolism of Fluvastatin can be decreased when combined with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Fluvastatin.
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Fluvastatin.
OlaparibThe metabolism of Fluvastatin can be decreased when combined with Olaparib.
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Fluvastatin.
OmeprazoleThe metabolism of Fluvastatin can be decreased when combined with Omeprazole.
OndansetronThe metabolism of Ondansetron can be decreased when combined with Fluvastatin.
OsimertinibThe serum concentration of Fluvastatin can be increased when it is combined with Osimertinib.
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Fluvastatin.
OxaprozinThe metabolism of Oxaprozin can be decreased when combined with Fluvastatin.
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Fluvastatin.
PalbociclibThe serum concentration of Fluvastatin can be increased when it is combined with Palbociclib.
PanobinostatThe metabolism of Fluvastatin can be decreased when combined with Panobinostat.
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Fluvastatin.
ParecoxibThe metabolism of Parecoxib can be decreased when combined with Fluvastatin.
ParoxetineThe metabolism of Fluvastatin can be decreased when combined with Paroxetine.
PazopanibFluvastatin may increase the hepatotoxic activities of Pazopanib.
Peginterferon alfa-2bThe serum concentration of Fluvastatin can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Fluvastatin can be increased when combined with Pentobarbital.
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Fluvastatin.
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Fluvastatin.
PhenindioneFluvastatin may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe metabolism of Fluvastatin can be increased when combined with Phenobarbital.
PhenprocoumonFluvastatin may increase the anticoagulant activities of Phenprocoumon.
PhenylbutazoneThe metabolism of Phenylbutazone can be decreased when combined with Fluvastatin.
PhenytoinThe serum concentration of Fluvastatin can be decreased when it is combined with Phenytoin.
PhenytoinThe metabolism of Phenytoin can be decreased when combined with Fluvastatin.
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Fluvastatin.
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Fluvastatin.
PitavastatinThe metabolism of Pitavastatin can be decreased when combined with Fluvastatin.
PosaconazoleThe metabolism of Fluvastatin can be decreased when combined with Posaconazole.
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Fluvastatin.
PravastatinThe metabolism of Pravastatin can be decreased when combined with Fluvastatin.
PrimidoneThe metabolism of Fluvastatin can be increased when combined with Primidone.
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Fluvastatin.
ProguanilThe metabolism of Proguanil can be decreased when combined with Fluvastatin.
PromazineThe metabolism of Fluvastatin can be decreased when combined with Promazine.
PropofolThe metabolism of Propofol can be decreased when combined with Fluvastatin.
PyrimethamineThe metabolism of Fluvastatin can be decreased when combined with Pyrimethamine.
QuazepamThe metabolism of Quazepam can be decreased when combined with Fluvastatin.
QuinidineThe metabolism of Fluvastatin can be decreased when combined with Quinidine.
QuinineThe metabolism of Fluvastatin can be decreased when combined with Quinine.
RabeprazoleThe metabolism of Fluvastatin can be decreased when combined with Rabeprazole.
RaltegravirRaltegravir may increase the myopathic rhabdomyolysis activities of Fluvastatin.
RanolazineThe metabolism of Fluvastatin can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Fluvastatin can be increased when combined with Rifabutin.
RifampicinThe metabolism of Fluvastatin can be increased when combined with Rifampicin.
RifapentineThe metabolism of Fluvastatin can be increased when combined with Rifapentine.
RitonavirThe metabolism of Fluvastatin can be decreased when combined with Ritonavir.
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Fluvastatin.
RolapitantThe metabolism of Fluvastatin can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Fluvastatin can be decreased when combined with Ropinirole.
RosiglitazoneThe metabolism of Rosiglitazone can be decreased when combined with Fluvastatin.
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Fluvastatin.
Salicylic acidThe metabolism of Salicylic acid can be decreased when combined with Fluvastatin.
SaquinavirThe metabolism of Fluvastatin can be decreased when combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Fluvastatin.
SecobarbitalThe metabolism of Fluvastatin can be increased when combined with Secobarbital.
SelegilineThe metabolism of Selegiline can be decreased when combined with Fluvastatin.
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Fluvastatin.
SertralineThe metabolism of Fluvastatin can be decreased when combined with Sertraline.
SildenafilThe metabolism of Fluvastatin can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Fluvastatin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Fluvastatin can be increased when it is combined with Simeprevir.
SitaxentanThe metabolism of Sitaxentan can be decreased when combined with Fluvastatin.
SorafenibThe metabolism of Fluvastatin can be decreased when combined with Sorafenib.
St. John's WortThe serum concentration of Fluvastatin can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Fluvastatin can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Sulfadiazine can be decreased when combined with Fluvastatin.
SulfamethoxazoleThe metabolism of Fluvastatin can be decreased when combined with Sulfamethoxazole.
SulfamoxoleThe metabolism of Sulfamoxole can be decreased when combined with Fluvastatin.
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Fluvastatin.
SulfisoxazoleThe metabolism of Fluvastatin can be decreased when combined with Sulfisoxazole.
SuprofenThe metabolism of Suprofen can be decreased when combined with Fluvastatin.
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Fluvastatin.
TapentadolThe metabolism of Tapentadol can be decreased when combined with Fluvastatin.
TelaprevirThe serum concentration of Fluvastatin can be increased when it is combined with Telaprevir.
TelithromycinThe metabolism of Fluvastatin can be decreased when combined with Telithromycin.
TemazepamThe metabolism of Temazepam can be decreased when combined with Fluvastatin.
TenoxicamThe metabolism of Tenoxicam can be decreased when combined with Fluvastatin.
TerbinafineThe metabolism of Fluvastatin can be decreased when combined with Terbinafine.
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Fluvastatin.
TeriflunomideThe metabolism of Fluvastatin can be decreased when combined with Teriflunomide.
TestosteroneThe metabolism of Testosterone can be decreased when combined with Fluvastatin.
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Fluvastatin.
TheophyllineThe metabolism of Theophylline can be decreased when combined with Fluvastatin.
ThiamylalThe metabolism of Thiamylal can be decreased when combined with Fluvastatin.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Fluvastatin.
ThioridazineThe metabolism of Fluvastatin can be decreased when combined with Thioridazine.
TicagrelorThe metabolism of Fluvastatin can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Fluvastatin can be decreased when combined with Ticlopidine.
TipranavirThe metabolism of Fluvastatin can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Fluvastatin can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Tolbutamide can be decreased when combined with Fluvastatin.
TolterodineThe metabolism of Tolterodine can be decreased when combined with Fluvastatin.
TorasemideThe metabolism of Torasemide can be decreased when combined with Fluvastatin.
TrabectedinFluvastatin may increase the myopathic rhabdomyolysis activities of Trabectedin.
TranylcypromineThe metabolism of Fluvastatin can be decreased when combined with Tranylcypromine.
TreprostinilThe metabolism of Treprostinil can be decreased when combined with Fluvastatin.
TretinoinThe metabolism of Tretinoin can be decreased when combined with Fluvastatin.
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Fluvastatin.
TrimethoprimThe metabolism of Fluvastatin can be decreased when combined with Trimethoprim.
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Fluvastatin.
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Fluvastatin.
ValdecoxibThe metabolism of Valdecoxib can be decreased when combined with Fluvastatin.
Valproic AcidThe metabolism of Fluvastatin can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Fluvastatin can be decreased when combined with Valsartan.
VenlafaxineThe metabolism of Fluvastatin can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Fluvastatin can be decreased when combined with Verapamil.
VicrivirocThe metabolism of Vicriviroc can be decreased when combined with Fluvastatin.
VismodegibThe metabolism of Vismodegib can be decreased when combined with Fluvastatin.
VoriconazoleThe metabolism of Fluvastatin can be decreased when combined with Voriconazole.
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Fluvastatin.
WarfarinFluvastatin may increase the anticoagulant activities of Warfarin.
XimelagatranThe metabolism of Ximelagatran can be decreased when combined with Fluvastatin.
ZafirlukastThe metabolism of Fluvastatin can be decreased when combined with Zafirlukast.
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Fluvastatin.
ZaltoprofenThe metabolism of Zaltoprofen can be decreased when combined with Fluvastatin.
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Fluvastatin.
ZileutonThe metabolism of Zileuton can be decreased when combined with Fluvastatin.
ZiprasidoneThe metabolism of Fluvastatin can be decreased when combined with Ziprasidone.
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Fluvastatin.
ZopicloneThe metabolism of Zopiclone can be decreased when combined with Fluvastatin.
Food Interactions
  • May be taken with or without food, but should be taken consistently.
  • When given with an evening meal, Cmax and AUC decreased while Tmax increased 2-fold

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Nadph binding
Specific Function:
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
Gene Name:
HMGCR
Uniprot ID:
P04035
Molecular Weight:
97475.155 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Podar K, Tai YT, Hideshima T, Vallet S, Richardson PG, Anderson KC: Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. doi: 10.1517/14728210802676278 . [PubMed:19249983 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Fischer V, Johanson L, Heitz F, Tullman R, Graham E, Baldeck JP, Robinson WT: The 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor fluvastatin: effect on human cytochrome P-450 and implications for metabolic drug interactions. Drug Metab Dispos. 1999 Mar;27(3):410-6. [PubMed:10064574 ]
  2. Toda T, Eliasson E, Ask B, Inotsume N, Rane A: Roles of different CYP enzymes in the formation of specific fluvastatin metabolites by human liver microsomes. Basic Clin Pharmacol Toxicol. 2009 Nov;105(5):327-32. doi: 10.1111/j.1742-7843.2009.00453.x. Epub 2009 Aug 6. [PubMed:19663817 ]
  3. Scripture CD, Pieper JA: Clinical pharmacokinetics of fluvastatin. Clin Pharmacokinet. 2001;40(4):263-81. [PubMed:11368292 ]
  4. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Kivisto KT, Niemi M, Schaeffeler E, Pitkala K, Tilvis R, Fromm MF, Schwab M, Eichelbaum M, Strandberg T: Lipid-lowering response to statins is affected by CYP3A5 polymorphism. Pharmacogenetics. 2004 Aug;14(8):523-5. [PubMed:15284534 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Fischer V, Johanson L, Heitz F, Tullman R, Graham E, Baldeck JP, Robinson WT: The 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor fluvastatin: effect on human cytochrome P-450 and implications for metabolic drug interactions. Drug Metab Dispos. 1999 Mar;27(3):410-6. [PubMed:10064574 ]
  2. Toda T, Eliasson E, Ask B, Inotsume N, Rane A: Roles of different CYP enzymes in the formation of specific fluvastatin metabolites by human liver microsomes. Basic Clin Pharmacol Toxicol. 2009 Nov;105(5):327-32. doi: 10.1111/j.1742-7843.2009.00453.x. Epub 2009 Aug 6. [PubMed:19663817 ]
  3. Scripture CD, Pieper JA: Clinical pharmacokinetics of fluvastatin. Clin Pharmacokinet. 2001;40(4):263-81. [PubMed:11368292 ]
  4. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Fischer V, Johanson L, Heitz F, Tullman R, Graham E, Baldeck JP, Robinson WT: The 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor fluvastatin: effect on human cytochrome P-450 and implications for metabolic drug interactions. Drug Metab Dispos. 1999 Mar;27(3):410-6. [PubMed:10064574 ]
  2. Toda T, Eliasson E, Ask B, Inotsume N, Rane A: Roles of different CYP enzymes in the formation of specific fluvastatin metabolites by human liver microsomes. Basic Clin Pharmacol Toxicol. 2009 Nov;105(5):327-32. doi: 10.1111/j.1742-7843.2009.00453.x. Epub 2009 Aug 6. [PubMed:19663817 ]
  3. Scripture CD, Pieper JA: Clinical pharmacokinetics of fluvastatin. Clin Pharmacokinet. 2001;40(4):263-81. [PubMed:11368292 ]
  4. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  6. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064 ]
  2. Scripture CD, Pieper JA: Clinical pharmacokinetics of fluvastatin. Clin Pharmacokinet. 2001;40(4):263-81. [PubMed:11368292 ]
  3. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A3
Uniprot ID:
P35503
Molecular Weight:
60337.835 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Glucuronosyltransferase activity
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol suggests it may play an important role in regulating the level and activity of these potent and active estrogen metabolites. Is also active with androsterone, hyodeoxycholic acid and tetrachlorocatechol...
Gene Name:
UGT2B7
Uniprot ID:
P16662
Molecular Weight:
60694.12 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Kopplow K, Letschert K, Konig J, Walter B, Keppler D: Human hepatobiliary transport of organic anions analyzed by quadruple-transfected cells. Mol Pharmacol. 2005 Oct;68(4):1031-8. Epub 2005 Jul 26. [PubMed:16046661 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Kopplow K, Letschert K, Konig J, Walter B, Keppler D: Human hepatobiliary transport of organic anions analyzed by quadruple-transfected cells. Mol Pharmacol. 2005 Oct;68(4):1031-8. Epub 2005 Jul 26. [PubMed:16046661 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Molecular Weight:
76709.98 Da
References
  1. Kopplow K, Letschert K, Konig J, Walter B, Keppler D: Human hepatobiliary transport of organic anions analyzed by quadruple-transfected cells. Mol Pharmacol. 2005 Oct;68(4):1031-8. Epub 2005 Jul 26. [PubMed:16046661 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Proton-dependent oligopeptide secondary active transmembrane transporter activity
Specific Function:
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. May constitute a major route for the absorption of protein digestion end-products.
Gene Name:
SLC15A1
Uniprot ID:
P46059
Molecular Weight:
78805.265 Da
References
  1. Ekins S, Johnston JS, Bahadduri P, D'Souza VM, Ray A, Chang C, Swaan PW: In vitro and pharmacophore-based discovery of novel hPEPT1 inhibitors. Pharm Res. 2005 Apr;22(4):512-7. Epub 2005 Apr 7. [PubMed:15846457 ]
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Drug created on June 13, 2005 07:24 / Updated on October 01, 2016 03:35